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1. 发明申请

WO2011149250A3 TRICARBONYL TECHNETIUM-99M OR RHENIUM-188 LABEL RING RGD DERIVATIVE, A PREPARATION METHOD THEREOF, AND A PHARMACEUTICAL COMPOSITION CONTAINING THE DERIVATIVE AS AN ACTIVE INGREDIENT FOR USE IN THE DIAGNOSIS OR TREATMENT OF ANGIOGENESIS-RELATED DISEAS 审中-公开
标题翻译： TRICARBONYL TECHNETIUM-99M或RHENIUM-188 LABEL RING RGD衍生物及其制备方法以及含有衍生物作为活性成分的药物组合物用于诊断或治疗血管发生相关疾病
公开(公告)号：WO2011149250A3
公开(公告)日：2012-03-22
申请号：PCT/KR2011003801
申请日：2011-05-24
申请人： SNU R&DB FOUNDATION , LEE BYUNG CHUL , KIM SANG EUN , KIM JI SUN , MOON BYUNG SEOK , JUNG JAE HO
发明人： LEE BYUNG CHUL , KIM SANG EUN , KIM JI SUN , MOON BYUNG SEOK , JUNG JAE HO
IPC分类号： C07D273/06 , A61K31/5395 , A61K51/04 , A61P35/00 , C07D498/06 , C07D498/16 , G01N33/60
CPC分类号： A61K51/088 , A61K51/082 , C07D273/06 , C07D498/06 , C07D498/16 , C07K7/64 , G01N33/574 , G01N33/60
摘要： The present invention relates to a tricarbonyl technetium-99m or rhenium-188 label ring RGD derivative, a preparation method thereof, and a pharmaceutical composition containing the derivative as an active ingredient for use in the diagnosis or treatment of angiogenesis-related diseases. The tricarbonyl technetium-99m or rhenium-188 label ring RGD derivative of the present invention has a high subnanomolar affinity to avß3 integrin (also called as a vitronectin receptor that is activated in an angiogenic action induced by a tumor, reflects a high tumor image after an animal in which cancer cells are transplanted received an initial intake of the tricarbonyl technetium-99m label ring RGD derivative, and acts exclusively upon cancer cells having selectively activated avß3 integrin because of a substantially low intake into the liver and intestines, compared to existing known radioactive isotope label ring RGD derivatives. These results show that the rhenium-188 label derivative, a therapeutic nuclide using the same precursor as used in the technetium-99m label, effectively inhibits the growth of a tumor and demonstrates therapeutic efficacy when administered via tail vein injection to an animal model of a tumor, compared to a case where only saline has been injected, thereby making it useful as a medicine for the diagnosis or treatment of angiogenesis-related diseases.
摘要翻译：本发明涉及三羰基锝-99m或铼-188标记环RGD衍生物，其制备方法和含有该衍生物作为用于诊断或治疗血管生成相关疾病的活性成分的药物组合物。本发明的三羰基锝-99m或铼-188标记环RGD衍生物对avß3整联蛋白（也称为在肿瘤诱导的血管生成作用中被激活的玻连蛋白受体）具有高亚纳摩尔亲和力，反映了肿瘤后高的肿瘤形象其中移植了癌细胞的动物接受三羰基锝-99m标记环RGD衍生物的初始摄入，并且仅与具有选择性活化的avß3整联蛋白的癌细胞起作用，因为与现有已知的这些结果表明，使用与锝-99m标记中使用相同前体的治疗性核素铼-188标签衍生物有效地抑制了肿瘤的生长并且通过尾静脉施用时表现出治疗功效注射到肿瘤的动物模型，与仅注射盐水的情况相比，t 因此可用作诊断或治疗血管生成相关疾病的药物。

2. 发明申请

WO2011030981A1 METHOD FOR PREPARING [18F]FALLYPRIDE WITH LOW BASE CONCENTRATION 审中-公开
标题翻译：用于制备具有低碱浓度的[18F] FALLYPRIDE的方法
公开(公告)号：WO2011030981A1
公开(公告)日：2011-03-17
申请号：PCT/KR2010/001351
申请日：2010-03-04
申请人： SNU R&DB FOUNDATION , KIM, Sang Eun , LEE, Byung Chul , MOON, Byung Seok , KIM, Yu Kyeong
发明人： KIM, Sang Eun , LEE, Byung Chul , MOON, Byung Seok , KIM, Yu Kyeong
IPC分类号： C07D207/14 , A61K31/40 , A61P21/00
CPC分类号： C07D207/09
摘要： A method for preparing [ 18 F]fallypride is disclosed, which comprises a first step for trapping a fluorine-18 to a polymer ion exchange cartridge; a second step for extraction of fluorine-18 by inputting low base concentrations: 5.0~25μL of 40% TBAHCO 3 or K2.2.2./K 2 CO 3 (5~25mg/0.5~3.0 mg) as a phase-transfer catalyst in a mixture of alcohol/water(1.0/0.2(v/v)) or alcohol as a solvent into the polymer ion exchange cartridge trapped by the fluorine-18; a third step for preparing a [ 18 F]fallypride product by removing the solvent from the trapped fluorine-18, by inputting tosylate precursor in CH 3 CN as a solvent into a reactor and by reacting the same for 5~35 minutes at 50~120°C; and a fourth step for preparing a pure [ 18 F]fallypride by purifying the prepared [ 18 F]fallypride product. The present invention makes it possible to improve the radiochemical yield of [ 18 F]fallypride, the improvement of which was a problem in the conventional automated method, by more than about 50% while reducing the preparation time by about 20 minutes. The present invention can be well applied to a clinical research by the positron emission tomography (PET).
摘要翻译：公开了一种制备[18 F]菲拉必利的方法，其包括将氟-18捕获到聚合物离子交换盒的第一步骤; 通过输入低碱浓度来提取氟-18的第二步：将5.0〜25μL40％TBAHCO 3或作为相转移催化剂的K2.2.2./K2CO3（5〜25mg / 0.5〜3.0mg）在醇的混合物中 /水（1.0 / 0.2（v / v））或醇作为溶剂进入被氟-18捕获的聚合物离子交换柱; 将通过在CH 3 CN中的甲苯磺酸酯前体作为溶剂输入反应器并通过在50〜120℃下反应5〜35分钟，通过从捕获的氟-18中除去溶剂来制备[18 F] fallypride产物的第三步骤 ; 以及通过纯化制备的[18 F] fallypride产物制备纯的[18 F] fallypride的第四步骤。通过本发明，可以提高常规自动化方法中的改善成为问题的[18F] fallypride的放射化学产率超过约50％，同时将制备时间缩短约20分钟。本发明可以很好地应用于正电子发射断层摄影（PET）的临床研究。

3. 发明申请

WO2008072903A1 METHOD OF PRODUCING SMALLPOX VACCINE IN THE FORM OF ATTENUATED VACCINIA VIRUS USING CELL CULTURE AND SMALLPOX VACCINE PRODUCED USING THE METHOD 审中-公开
标题翻译：使用细胞培养和使用该方法生产的小型疫霉素的减毒疫苗的形式制造小型疫苗的方法
公开(公告)号：WO2008072903A1
公开(公告)日：2008-06-19
申请号：PCT/KR2007/006483
申请日：2007-12-12
申请人： CJ CHEILJEDANG CORP. , KANG, Joon-Mo , SONG, Geun-Seog , MHA, Sang-Hyun , KIM, Hyun-Ah , KIM, Ah-Mee , PARK, Hyung-Ki , AHN, Jee-Won , MOON, Byung-Seok , KIM, Young-Gi , LEE, Chung-Min , YOUN, Sang-Jun , MIN, Mi-Kyung
发明人： KANG, Joon-Mo , SONG, Geun-Seog , MHA, Sang-Hyun , KIM, Hyun-Ah , KIM, Ah-Mee , PARK, Hyung-Ki , AHN, Jee-Won , MOON, Byung-Seok , KIM, Young-Gi , LEE, Chung-Min , YOUN, Sang-Jun , MIN, Mi-Kyung
IPC分类号： A61K39/42
CPC分类号： C12N7/00 , A61K39/12 , A61K39/285 , A61K2039/545 , C12N2710/24134 , C12N2710/24164
摘要： Provided are a method of producing a smallpox vaccine in the form of an attenuated vaccinia virus, the method comprising: inoculating an attenuated New York City Board of Health (NYCBOH) strain of vaccinia virus into cells derived from humans and culturing the infected cells to proliferate the viruses, and recovering the attenuated vaccinia virus from the culture, and an immunogenic composition for preventing or curing smallpox, comprising the attenuated vaccinia virus produced using the method and a stabilizer.
摘要翻译：本发明提供一种以减毒痘苗病毒的形式生产天花疫苗的方法，该方法包括：将一种减毒的纽约市卫生局（NYCBOH）痘苗病毒株接种到源自人的细胞中并培养感染的细胞以增殖病毒和从培养物中回收减毒的痘苗病毒，以及用于预防或治疗天花的免疫原性组合物，其包含使用该方法产生的减毒痘苗病毒和稳定剂。

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